Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1251068

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H]prazosin from human adrenergic Alpha-1D expressed in CHO cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Alpha-1D adrenergic receptor (CHEMBL223)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationships in 1,4-benzodioxan-related compounds. 10. Novel α1-adrenoreceptor antagonists related to openphendioxan: synthesis, biological evaluation, and α1d computational study.
Carrieri A, Piergentili A, Del Bello F, Giannella M, Pigini M, Leonardi A, Fanelli F, Quaglia W.
Bioorg Med Chem (2010) 18 : 7065 -7077
PubMed 20801662 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 8.80 10.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL43116 1 10.17
CHEMBL1254582 1 9.75
CHEMBL1254742 1 9.41
CHEMBL1254743 1 9.29
CHEMBL25554 1 9.29
CHEMBL1254828 1 9.13
CHEMBL1254829 1 9.04
CHEMBL1254659 1 8.92
CHEMBL1254660 1 8.56
CHEMBL1254914 1 8.43
CHEMBL1254915 1 8.40
CHEMBL1255002 1 8.15
CHEMBL1255003 1 7.85
CHEMBL1255085 1 7.82
CHEMBL1255086 1 7.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL43116 Ki = 0.06761 nM 10.17
CHEMBL1254582 Ki = 0.1778 nM 9.75
CHEMBL1254742 Ki = 0.389 nM 9.41
CHEMBL1254743 Ki = 0.5129 nM 9.29
CHEMBL25554 Ki = 0.5129 nM 9.29
CHEMBL1254828 Ki = 0.7413 nM 9.13
CHEMBL1254829 Ki = 0.912 nM 9.04
CHEMBL1254659 Ki = 1.202 nM 8.92
CHEMBL1254660 Ki = 2.754 nM 8.56
CHEMBL1254914 Ki = 3.715 nM 8.43
CHEMBL1254915 Ki = 3.981 nM 8.40
CHEMBL1255002 Ki = 7.079 nM 8.15
CHEMBL1255003 Ki = 14.13 nM 7.85
CHEMBL1255085 Ki = 15.14 nM 7.82
CHEMBL1255086 Ki = 17.78 nM 7.75